Bromocriptine

Bromocriptine is used to treat acromegaly and conditions associated with hyperprolactinemia like amenorrhea, infertility, and hypogonadism, prolactin-secreting adenomas; it is also used to prevent ovarian hyperstimulation syndrome.[3][4][5]

It is also used to treat Parkinson's disease.[3]

Since the late 1980s it has been used, off-label, to reduce the symptoms of cocaine withdrawal but the evidence for this use is poor.[6]

A quick-release formulation of bromocriptine, Cycloset, is also used to treat type 2 diabetes.[7][8][9] When administered within 2 hours of awakening, it increases hypothalamic dopamine level and as a result decreases hepatic glucose production. It therefore acts as an adjunct to diet and exercise to improve glycemic control.[10]

Most frequent side effects are nausea, orthostatic hypotension, headaches, and vomiting through stimulation of the brainstem vomiting centre.[11] Vasospasms with serious consequences such as myocardial infarction and stroke that have been reported in connection with the puerperium, appear to be extremely rare events.[12] Peripheral vasospasm (of the fingers or toes) can cause Raynaud's Phenomenon. Bromocriptine use has been anecdotally associated with causing or worsening psychotic symptoms (its mechanism is in opposition of most antipsychotics, whose mechanisms generally block dopamine receptors).[13] Pulmonary fibrosis has been reported when bromocriptine was used in high doses for the treatment of Parkinson's disease.[14]

Use to suppress milk production after childbirth was reviewed in 2014 and it was concluded that in this context a causal association with serious cardiovascular, neurological or psychiatric events could not be excluded with an overall incidence rate estimated to range between 0.005% and 0.04%. Additional safety precautions and stricter prescribing rules were suggested based on the data.[15][16] It is a bile salt export pump inhibitor.[17]

After long-term use of dopamine agonists, a withdrawal syndrome may occur during dose reduction or discontinuation with the following possible side effects: anxiety, panic attacks, dysphoria, depression, agitation, irritability, suicidal ideation, fatigue, orthostatic hypotension, nausea, vomiting, diaphoresis, generalized pain, and drug cravings. For some individuals, these withdrawal symptoms are short-lived and they make a full recovery, for others a protracted withdrawal syndrome may occur with withdrawal symptoms persisting for months or years.[18]

Bromocriptine is a potent agonist at dopamine D2 receptors[19] and various serotonin receptors. It also inhibits the release of glutamate, by reversing the glutamate GLT1 transporter.[20]

Bromocriptine agonizes the following monoamine receptors:[21]

• Dopamine D₁ family
  • D₁ (K_i=682 nM)
  • D₅ (K_i=496 nM)
• Dopamine D₂ family
  • D₂ (K_i=2.96 nM)
  • D₃ (K_i=5.42 nM)
  • D₄ (K_i=328 nM)
• Serotonin 5-HT
  • 5-HT_1A (K_i=12.9 nM)
  • 5-HT_1B (K_i=355 nM)
  • 5-HT_1D (K_i=10.7 nM)
  • 5-HT_2A (K_i=107 nM)
  • 5-HT_2B (K_i=56.2 nM)
  • 5-HT_2C (K_i=741 nM)
  • 5-HT₆ (K_i=33 nM)
• Adrenergic α family
  • α_1A (K_i=4.17 nM)
  • α_1B (K_i=1.38 nM)
  • α_1D (K_i=1.12 nM)
  • α_2A (K_i=11.0 nM)
  • α_2B (K_i=34.7 nM)
  • α_2C (K_i=28.2 nM)
• Adrenergic β family
  • β₁ (K_i=589 nM)
  • β₂ (K_i=741 nM)

Like all ergopeptides, bromocriptine is a cyclol; two peptide groups of its tripeptide moiety are crosslinked, forming the >N-C(OH)< juncture between the two rings with the amide functionality.

Bromocriptine is a semisynthetic derivative of a natural ergot alkaloid, ergocryptine (a derivative of lysergic acid), which is synthesized by bromination of ergocryptine using N-bromosuccinimide.[22][23]

Bromocriptine was discovered by scientists at Sandoz in 1965 and was first published in 1968; it was first marketed under the brand name Parlodel.[24][25]

A quick-release formulation of bromocriptine was approved by the FDA in 2009.[26]

As of July 2017, bromocriptine was marketed under many brand names worldwide, including Abergin, Barlolin, Brameston, Brocriptin, Brom, Broma-Del, Bromergocryptine, Bromergon, Bromicon, Bromocorn, Bromocriptin, Bromocriptina, Bromocriptine, Bromocriptine mesilate, Bromocriptine mesylate, Bromocriptine methanesulfonate, Bromocriptini mesilas, Bromocriptinmesilat, Bromodel, Bromokriptin, Bromolac, Bromotine, Bromtine, Brotin, Butin, Corpadel, Cripsa, Criptine, Criten, Cycloset, Degala, Demil, Deparo, Deprolac, Diacriptin, Dopagon, Erenant, Grifocriptina, Gynodel, kirim, Kriptonal, Lactodel, Medocriptine, Melen, Padoparine, Palolactin, Parlodel, Pravidel, Proctinal, Ronalin, Semi-Brom, Serocriptin, Serocryptin, Suplac, Syntocriptine, Umprel, Unew, Updopa, Upnol B, and Volbro.[1]

As of July 2017 it was also marketed as a combination drug with metformin as Diacriptin-M, and as a veterinary drug under the brand Pseudogravin.[1]

• Cabergoline

• www.AcromegalyCommunity.com: Emotional and communal support for those touched by Acromegaly- page discussing drug, side effects, and prescription programs
• MedlinePlus DrugInfo medmaster-a682079
• https://www.drugs.com/pro/bromocriptine.html